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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
 
 

New progesterone receptor antagonists: 3,3-disubstituted-5-aryloxindoles.

A new series of 3,3-disubstituted-5-aryloxindoles has been synthesized and evaluated for progesterone receptor antagonist ( PR) activity in a T47D cell alkaline phosphatase assay and for their ability to bind PR in competition binding studies. In this communication, the synthesis and structure-activity relationships (SARs) of various 3,3-substituents are discussed where it is clear that small alkyl and spiroalkyl groups are required to achieve better PR antagonist activity.[1]

References

  1. New progesterone receptor antagonists: 3,3-disubstituted-5-aryloxindoles. Fensome, A., Bender, R., Cohen, J., Collins, M.A., Mackner, V.A., Miller, L.L., Ullrich, J.W., Winneker, R., Wrobel, J., Zhang, P., Zhang, Z., Zhu, Y. Bioorg. Med. Chem. Lett. (2002) [Pubmed]
 
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